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    BIS-H-PHOSPHINIC ACID DERIVATIVES AS PRECURSORS TO THERAPEUTIC BISPHOSPHONATES AND USES THEREOF
    2.
    发明申请
    BIS-H-PHOSPHINIC ACID DERIVATIVES AS PRECURSORS TO THERAPEUTIC BISPHOSPHONATES AND USES THEREOF 失效
    BIS-H-磷酸衍生物作为治疗性二磷酸酯的前驱体及其用途

    公开(公告)号：US20040116673A1

    公开(公告)日：2004-06-17

    申请号：US10318731

    申请日：2002-12-13

    申请人： Texas Christian University

    发明人： Jean-Luc Montchamp ,  Sylvine Deprele

    IPC分类号： C07F009/22 ,  C07J001/00

    CPC分类号： C07J1/00 ,  A61K47/548 ,  A61K47/643 ,  C07F9/485

    摘要： A novel class of compounds, i.e., 1,1-bis-H-phosphinates (or 1,1-bis-H-phosphinic acid derivatives) are provided. Also provided are novel methods for producing 1,1-bis-H-phosphinates and 1,1-bis-H-phosphinate conjugates. These compounds and conjugates are used as precursors of bisphosphonates and bisphosphonate conjugates, respectively, or as prodrugs directly for treating bone-related and various other diseases.

    摘要翻译： 提供了一类新颖的化合物，即1,1-双-H-次膦酸盐（或1,1-双H-次膦酸衍生物）。 还提供了用于生产1,1-双-H-次膦酸盐和1,1-双-H-次膦酸盐共轭物的新方法。 这些化合物和缀合物分别用作双膦酸盐和二膦酸盐缀合物的前体，或直接用作治疗骨相关和各种其它疾病的前药。

    Fluorinated and halogenated phosphinic acids and their active metal derivatives
    3.
    发明申请
    Fluorinated and halogenated phosphinic acids and their active metal derivatives 审中-公开
    氟化和卤代次膦酸及其活性金属衍生物

    公开(公告)号：US20030189193A1

    公开(公告)日：2003-10-09

    申请号：US10227301

    申请日：2002-08-26

    发明人： Robert M. Mininni ,  Yousef Mohajer ,  Anthony Garito ,  Anna A. Panackal ,  Joseph A. Virgilio

    IPC分类号： G02F001/01 ,  C07F009/22 ,  C07F009/28 ,  C07F009/02 ,  G02F001/00

    CPC分类号： C07F9/301 ,  C07C17/093 ,  C07F9/3211 ,  C07C25/02

    摘要： Compounds of formula (I), methods of making and method of using (including optical compositions and devices) are provided. The compounds are 1 where A1 is selected from O and S; A2 is selected from nullOH, nullSH, and nullOR3; Rf and Rf1 can be the same or different, can be branched or unbranched, can be linked to form cyclic or extended structures, and are selected from halogenated alkyl, halogenated aryl, halogenated cyclic alkyl, halogenated arylalkyl, halogenated alkylaryl, halogenated polyether, halogenated thioether, halogenated ether thioether, halogenated aklyl amino groups, halogenated alkylene, halogenated silylene, halogenated siloxanes, halogenated silazanes, halogenated olefins, perfluorinated C1-20 alkyl, perfuorinated C1-6 alkyl C1-10 alkyl ethers, n-C8F17, n-C6F13, n-C4F9, n-C2F5, (CF3)2CF(CF2)4, n-C10F21, n-C12F25, (CF3)2CF(CF2)6, and (CF3)2CFO(CF2)2; and R3 can be branched or unbranched and is selected from C1-15 alkyl, C3-15 aryl, C4-15 alkylaryl, and C4-15 arylalkyl. Wherein, (i) if Rf and Rf1 are the same and selected from n-C2F5, n-C4F9, n-C6F13, n-C7F15, and n-C8F17, then A1 is not O; (ii) if Rf and Rf1 are the same and selected from n-C2F5, n-C4F9, n-C6F13, n-C7F15, and n-C8F17, then A2 is not nullOH; and (iii) if A1 is O, and if Rf and Rf1 are the same and selected from n-C6F13, n-C7F15 and n-C8F17, then A2 is not nullOCH3.

    摘要翻译： 提供式（I）化合物，制备方法和使用方法（包括光学组合物和装置）。 化合物是A1选自O和S的化合物; A 2选自-OH，-SH和-OR 3; Rf和Rf1可以相同或不同，可以是支链或非支链的，可以连接形成环状或延伸结构，并且选自卤代烷基，卤代芳基，卤代环烷基，卤代芳基烷基，卤代烷基芳基，卤代聚醚，卤代 硫醚，卤代醚硫醚，卤代烷基氨基，卤代亚烷基，卤代亚甲硅氧烷，卤代硅氧烷，卤化硅氮烷，卤代烯烃，全氟化C 1-20烷基，全氟化C 1-6烷基C 1-10烷基醚，n-C 8 F 17，n-C 6 F 13 （CF 3）2 CFF（CF 2）2，（C 3 F 5）2 CF 3，CF 2） 并且R 3可以是支链或非支链的，并且选自C1-15烷基，C3-15芳基，C4-15烷基芳基和C4-15芳基烷基。 其中，（i）如果Rf和Rf1相同且选自n-C2F5，n-C4F9，n-C6F13，n-C7F15和n-C8F17，则A1不为O; （ii）如果Rf和Rf1相同且选自n-C2F5，n-C4F9，n-C6F13，n-C7F15和n-C8F17，则A

    Process for the preparation of N-phosphonomethylglycine
    4.
    发明申请
    Process for the preparation of N-phosphonomethylglycine 失效
    N-膦酰基甲基甘氨酸的制备方法

    公开(公告)号：US20030166966A1

    公开(公告)日：2003-09-04

    申请号：US10368577

    申请日：2003-02-20

    发明人： Christian Wulff ,  Stefan Orsten ,  Alfred Oftring

    IPC分类号： C07F009/22 ,  C07F009/28

    CPC分类号： C07F9/4093 ,  C07F9/3813

    摘要： The present invention relates to a process for the preparation of N-phosphonomethylglycine by reacting a hexahydrotriazine derivative with a triacyl phosphite. The process gives N-phosphonomethylglycine in high yield and in a simple and inexpensive manner.

    摘要翻译： 本发明涉及通过使六氢三嗪衍生物与亚磷酸三酰基酯反应来制备N-膦酰基甲基甘氨酸的方法。 该方法以高产率和简单且廉价的方式得到N-膦酰基甲基甘氨酸。

    Process for preparing methylene biosphosphonic and salts
    8.
    发明申请
    Process for preparing methylene biosphosphonic and salts 有权
    制备亚甲基双膦和盐的方法

    公开(公告)号：US20040171870A1

    公开(公告)日：2004-09-02

    申请号：US10725820

    申请日：2003-12-01

    申请人： AstraZeneca UK Limited, a London corporation

    发明人： Mark Purdie

    IPC分类号： C07F009/22

    CPC分类号： C07F9/3856 ,  C07F9/3843

    摘要： A process for the preparation of salts of substituted or unsubstituted methylene bisphosphonic acids by hydrolysing the corresponding acid ester with hydrochloric acid, removing water from the acid azeotropically prior to addition of an amine or a base to produce the resultant salt in good yield.

    摘要翻译： 通过用盐酸水解相应的酸酯，在加入胺或碱之前共沸除去酸中的水来制备取代或未取代的亚甲基双膦酸的盐的方法，以高产率得到所得的盐。

    Novel aminoindanes
    9.
    发明申请
    Novel aminoindanes 审中-公开
    新型氨基茚满

    公开(公告)号：US20040152670A1

    公开(公告)日：2004-08-05

    申请号：US10763934

    申请日：2004-01-23

    发明人： Kenneth Curry

    IPC分类号： A61K031/66 ,  A61K031/69 ,  C07F009/22 ,  C07F005/02

    CPC分类号： C07D235/02 ,  C07C229/36 ,  C07C229/46 ,  C07C229/50 ,  C07C255/42 ,  C07C255/47 ,  C07C2602/08 ,  C07D233/76

    摘要： The present invention relates to therapeutically active novel aminoindanes of formula (I). Also provided is a method of preparing compounds of formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

    摘要翻译： 本发明涉及式（I）的治疗活性的新型氨基茚满。 还提供了制备式（I）化合物的方法和包含该化合物的药物组合物。 新型化合物作为代谢型谷氨酸受体的调节剂，因此可用于治疗与代谢型谷氨酸受体系统相关的中枢神经系统疾病。

    Combrestatin a-1 phosphate and combrestatin b-1 phosphate prodrugs
    10.
    发明申请
    Combrestatin a-1 phosphate and combrestatin b-1 phosphate prodrugs 有权
    Combrestatin a-1磷酸酯和combrestatin b-1磷酸酯前药

    公开(公告)号：US20030220298A1

    公开(公告)日：2003-11-27

    申请号：US10258672

    申请日：2002-10-25

    发明人： George R. Pettit ,  John W. Lippert

    IPC分类号： C07F009/22 ,  C07F009/28 ,  A61K031/675

    CPC分类号： C07D213/82 ,  A61K47/55 ,  C07C255/43 ,  C07D217/20 ,  C07D295/027 ,  C07D453/04 ,  C07F9/12

    摘要： The present invention relates to the syntheses and structural elucidation of Combretastatin A1-Phosphate Prodrugs and Combretastatin B1-Phosphate Prodrugs and the utilization of those prodrugs in the treatment of neoplastic diseases. The prodrugs described herein have the structure: Combretastin A-1 Phosphate Prodrug (I) and Combretastin B-1 Phosphate Prodrug (II). 1

    摘要翻译： 本发明涉及Combretastatin A1-Phosphate Prodrugs和Combretastatin B1-Phosphate Prodrugs的合成和结构阐明以及这些前药在治疗肿瘤性疾病中的应用。 本文所述的前药具有以下结构：Combretastin A-1磷酸盐前体药物（I）和Combretastin B-1磷酸盐前体药物（II）。